A cell-permeable 7-chloroindolylmethyl-hydantoin that exhibits highly RIP1-selective inhibitory activity among >400 human kinases and is superior to its structural analog Necrostatin-1 in blocking RIP1-dependent necroptosis due to improved potency (EC50 = 206nM vs. 494nM with Nec-1 for protecting FADD-deficient Jurkat from 30h 10ng/mL TNF-alpha-induced death), selectivity, metabolic stability, as well as reduced in vitro and in vivo toxicity. Reported to be blood-brain barrier permeable in mice and be efficacious in reducing brain infarct size when applied via intracerebroventricular injections in a murine MCAO model in vivo (8nMol/2uL/mouse).
Synonyms:7-Cl-O-MH-Trp, Nec-1s, Nec-1 stable, RIPK1 Inhibitor II, Receptor-Interacting Protein 1 Inhibitor II, Necrosis Inhibitor IV, 5-((7-Chloro-1H-indol-3-yl)methyl)-3-methyl-2,4-imidazolidinedione, 5-((7-Chloro-1H-indol-3-yl)methyl)-3-methylimidazolidine-2,4-dione, 7N-1
Molecular Formula:C₁₃H₁₂ClN₃O₂
Primary Target:RIP1
Solubility:DMSO (100mg/ml). Use only fresh DMSO for reconstitution.
Purity:≥95% (HPLC)
Form:Supplied as an off-white to pale yellow solid.
Storage and Stability:Store at -20°C under inert atmosphere. For maximum recovery of product, centrifuge the original vial prior to removing the cap.
仕様
Size:10mg
Grade:Highly Purified
Purity:≥95% (HPLC)
Form:Supplied as an off-white to pale yellow solid.